2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Apoptosis
  3. Phosphatase PI3K TNF Receptor
  4. AQX-016A

AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research.

For research use only. We do not sell to patients.

AQX-016A

AQX-016A Chemical Structure

CAS No. : 849669-54-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

AQX-016A Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research[1][2].

IC50 & Target

CD40

 

PI3K

 

In Vitro

AQX-016A (5 μg/mL, 30 min) inhibits the PI3K-mediated increase in intracellular PIP3 levels, and reduces PIP3 levels through activation of a 5 'phosphatase enzyme[1].
AQX-01 6A (0-5 μg/mL, 30 min) inhibits LPS-induced PKB phosphorylation in a SHIP dependent manner[1].
AQX-016A (0-5 μg/mL, 2 h) significantly inhibits TNFa in both J774 and peritoneal macrophages at both 1 and 5 μg/mL[1].
AQX-016A (0-6 μg/mL, 30 min) requires SHIP to maximally inhibit TNFa production in BMDM, selectively inhibits TNF production from SHIP1+/+ but not SHIP1-/- macrophages[1].
AQX-016A (0-5 μg/mL, 0-90 min) inhibits TNFa translation[1].
AQX-016A (0-15 μM, 30 min) increases SHIP1 enzyme activity in vitro and in intact cells, inhibits macrophage and mast-cell activation[2].
AQX-016A (15 μM, 30 min) inhibits immune cell activation, and inhibits PI3K-dependent macrophage and mast-cell responses in a SHIP-dependent manner[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AQX-016A Related Antibodies

Western Blot Analysis

Cell Line: SHIP1+/+ and SHIP1-/- mast cells[2]
Concentration: 0, 3, 6, 15, 30 μM
Incubation Time: 30 min
Result: Inhibited PIP3-regulated intracellular signal transduction events in SHIP-expressing hematopoietic cells, but not in SHIP-deficient hematopoietic or nonhematopoietic cells. Preferentially inhibited, in a dose-dependent manner, LPS-stimulated PKB phosphorylation in SHIP1+/+ but not in SHIP1-/-macrophages, and inhibited the phosphorylation of PKB, p38MAPK and extracellular signal-regulated kinase (ERK) in SHIP1+/+ but not in SHIP1-/- mast cells.
In Vivo

AQX-016A (20 mg/kg, Orally, once) significantly inhibits plasma TNFa levels, and inhibits inflammation in a mouse model endotoxemia[1][2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

328.49

Formula

C22H32O2
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

OC1=C(O)C2=C(C(C)=C1)[C@]3(C)CC[C@](C(C)(C)CCC4)([H])[C@@]4(C)[C@@]3([H])C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (304.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 66 mg/mL (200.92 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0442 mL 15.2212 mL 30.4423 mL
5 mM 0.6088 mL 3.0442 mL 6.0885 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.51%

SDS (252 KB)

COA (253 KB) HNMR (296 KB) RP-HPLC (258 KB) LCMS (117 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.0442 mL 15.2212 mL 30.4423 mL 76.1058 mL
5 mM 0.6088 mL 3.0442 mL 6.0885 mL 15.2212 mL
10 mM 0.3044 mL 1.5221 mL 3.0442 mL 7.6106 mL
15 mM 0.2029 mL 1.0147 mL 2.0295 mL 5.0737 mL
20 mM 0.1522 mL 0.7611 mL 1.5221 mL 3.8053 mL
25 mM 0.1218 mL 0.6088 mL 1.2177 mL 3.0442 mL
30 mM 0.1015 mL 0.5074 mL 1.0147 mL 2.5369 mL
40 mM 0.0761 mL 0.3805 mL 0.7611 mL 1.9026 mL
50 mM 0.0609 mL 0.3044 mL 0.6088 mL 1.5221 mL
60 mM 0.0507 mL 0.2537 mL 0.5074 mL 1.2684 mL
80 mM 0.0381 mL 0.1903 mL 0.3805 mL 0.9513 mL
100 mM 0.0304 mL 0.1522 mL 0.3044 mL 0.7611 mL
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AQX-016A Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AQX-016A849669-54-1PhosphatasePI3KTNF ReceptorPhosphoinositide 3-kinaseTumor Necrosis Factor ReceptorTNFROrally activeInflammatory diseasesSepticemiamantle cell lymphoma (MCL)Hematopoietic malignancies multiple myelomaEndotoxemiaInhibitorinhibitorinhibit

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